Sarizotan

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Sarizotan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

351862-32-3

EMD 128130

Sarizotan (EMD 128130) 是具有口服活性的5-HT_1A受体和多巴胺受体的激动剂，其IC₅₀值分别为 6.5 nM (rat 5-HT_1A)、 0.1 nM (human 5-HT_1A)、15.1 nM (rat D₂)、17 nM (human D₂)、6.8 nM (human D₃) 和 2.4 nM (human D_4.2)。

生物活性

Sarizotan (EMD 128130) is an orally active serotonin5-HT_1Areceptoranddopamine receptoragonist. Sarizotan (EMD 128130) exhibitsIC₅₀values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively^[1].

IC₅₀& Target^[1]

5-HT_1AReceptor

6.5 nM (IC₅₀, rat)

5-HT_1AReceptor

0.1 nM (IC₅₀, human)

rD₂Receptor

15.1 nM (IC₅₀, rat)

D₃Receptor

6.8 nM (IC₅₀, human)

5-HT_1BReceptor

600 nM (IC₅₀, rat)

5-HT_1DReceptor

500 nM (IC₅₀, calf)

5-HT_2AReceptor

960 nM (IC₅₀, rat, agonist site)

5-HT_2AReceptor

587 nM (IC₅₀, human, antagonist site)

5-HT_2BReceptor

108 nM (IC₅₀, human)

5-HT_2CReceptor

800 nM (IC₅₀, pig)

5-HT₃Receptor

3500 nM (IC₅₀, NG 108 cells)

5-HT_5AReceptor

313 nM (IC₅₀, human)

5-HT₆Receptor

3300 nM (IC₅₀, human)

5-HT₇Receptor

10 nM (IC₅₀, human)

hD_4.2Receptor

2.4 nM (IC₅₀)

hD₂Receptor

17 nM (IC₅₀)

体外研究
(In Vitro)

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC₅₀value of 150 nM (E_max40% at 1 mM)^[1].

体内研究
(In Vivo)

Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex^[1].
Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease^[1].
Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats^[2].

Animal Model:	Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)^[2].
Dosage:	1 ng, 10 ng and 1 μg in 0.3 μL solution.
Administration:	Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days.
Result:	On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).

Clinical Trial

分子量

348.41

性状

Viscous liquid

Formula

C₂₂H₂₁FN₂O

CAS 号

351862-32-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(287.02 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.8702 mL	14.3509 mL	28.7018 mL
5 mM	0.5740 mL	2.8702 mL	5.7404 mL
10 mM	0.2870 mL	1.4351 mL	2.8702 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。